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EPZ020411

Chemical Structure : EPZ020411

CAS No.: 1700663-41-7

EPZ020411 (EPZ-020411)

Catalog No.: PC-43300Not For Human Use, Lab Use Only.

EPZ020411 is a potent, selective PRMT6 inhibitor with IC50 of 10 nM, displays 10-fold and 20-fold selectivity over PRMT1/8, and >100-fold over other histone methyltransferases (PRMT3/4/5/7).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

EPZ020411 is a potent, selective PRMT6 inhibitor with IC50 of 10 nM, displays 10-fold and 20-fold selectivity over PRMT1/8, and >100-fold over other histone methyltransferases (PRMT3/4/5/7).
EPZ020411 dose-dependently decreases H3R2 methylation A375 cell line with IC50 of 0.637 uM, with no affect levels of PRMT6 expression.
EPZ020411 exhibits good bioavailability following subcutaneous dosing in rats making it a suitable tool for potential in vivo target validation studies.

Physicochemical Properties

M.Wt 442.5942
Formula C25H38N4O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1,2-Ethanediamine, N1,N2-dimethyl-N1-[[3-[4-[[trans-3-[2-(tetrahydro-2H-pyran-4-yl)ethoxy]cyclobutyl]oxy]phenyl]-1H-pyrazol-4-yl]methyl]-

References

1. Mitchell LH, et al. ACS Med Chem Lett. 2015 Apr 6;6(6):655-9.

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